1219630-54-2Relevant academic research and scientific papers
HCV NS5A replication complex inhibitors. Part 5: Discovery of potent and pan-genotypic glycinamide cap derivatives
Belema, Makonen,Nguyen, Van N.,St. Laurent, Denis R.,Lopez, Omar D.,Qiu, Yuping,Good, Andrew C.,Nower, Peter T.,Valera, Lourdes,O'Boyle II, Donald R.,Sun, Jin-Hua,Liu, Mengping,Fridell, Robert A.,Lemm, Julie A.,Gao, Min,Knipe, Jay O.,Meanwell, Nicholas A.,Snyder, Lawrence B.
, p. 4428 - 4435 (2013/07/26)
The isoquinolinamide series of HCV NS5A inhibitors exemplified by compounds 2b and 2c provided the first dual genotype-1a/1b (GT-1a/1b) inhibitor class that demonstrated a significant improvement in potency toward GT-1a replicons compared to that of the initial program lead, stilbene 2a. Structure-activity relationship (SAR) studies that uncovered an alternate phenylglycine-based cap series that exhibit further improvements in virology profile, along with some insights into the pharmacophoric elements associated with the GT-1a potency, are described.
